Hedgehog/Smoothened

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1082 Vismodegib (GDC-0449) <1 mg/mL 84 mg/mL <1 mg/mL
S1146 Cyclopamine <1 mg/mL <1 mg/mL 2 mg/mL
S2151 Sonidegib (Erismodegib, NVP-LDE225) <1 mg/mL 97 mg/mL 97 mg/mL
S2157 Taladegib (LY2940680) <1 mg/mL 5 mg/mL 2 mg/mL
S3042 Purmorphamine <1 mg/mL 4 mg/mL <1 mg/mL
S4747 Jervine <1 mg/mL 5 mg/mL 2 mg/mL
S8249 HPI-4 (Ciliobrevin A) <1 mg/mL 71 mg/mL 1 mg/mL
S8200 MK-4101 <1 mg/mL 98 mg/mL 60 mg/mL
S2777 PF-5274857 93 mg/mL 93 mg/mL <1 mg/mL
S8075 GANT61 <1 mg/mL <1 mg/mL 12 mg/mL
S7092 SANT-1 <1 mg/mL 21 mg/mL 20 mg/mL
S7138 BMS-833923 <1 mg/mL 95 mg/mL <1 mg/mL
S7779 Smoothened Agonist (SAG) HCl 100 mg/mL 71 mg/mL 40 mg/mL
S7160 Glasdegib (PF-04449913) <1 mg/mL 47 mg/mL <1 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1082

Vismodegib (GDC-0449)

Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.

S2157

Taladegib (LY2940680)

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

S4747New

Jervine

Jervine is an inhibitor of Hedgehog signaling (IC50=500-700 nM) that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.

S8249New

HPI-4 (Ciliobrevin A)

HPI-4 (Ciliobrevin A) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.

S8200New

MK-4101

MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.

S8075

GANT61

GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

S7160

Glasdegib (PF-04449913)

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

S3042

Purmorphamine

Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

S7779

Smoothened Agonist (SAG) HCl

Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

S1146

Cyclopamine

Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

S2151

Sonidegib (Erismodegib, NVP-LDE225)

Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.

S2777

PF-5274857

PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.

S7092

SANT-1

SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.

S7138

BMS-833923

BMS-833923 is an orally bioavailable Smoothened antagonist. Phase 2.

Catalog No. Information Product Use Citations Product Validations
S1082

Vismodegib (GDC-0449)

Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.

S2157

Taladegib (LY2940680)

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

S4747New

Jervine

Jervine is an inhibitor of Hedgehog signaling (IC50=500-700 nM) that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.

S8249New

HPI-4 (Ciliobrevin A)

HPI-4 (Ciliobrevin A) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.

S8200New

MK-4101

MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.

S8075

GANT61

GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

S7160

Glasdegib (PF-04449913)

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

Catalog No. Information Product Use Citations Product Validations
S1146

Cyclopamine

Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

2015, 10.1038/nature14325

2012, 72(9):2262-74

2013, 4(10):1698-1711

S2151

Sonidegib (Erismodegib, NVP-LDE225)

Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.

2013, 9(4):247-9

2015, 21(20):4686-97

2015, 34(29):3770-9

S2777

PF-5274857

PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.

S7092

SANT-1

SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.

S7138

BMS-833923

BMS-833923 is an orally bioavailable Smoothened antagonist. Phase 2.

2015, 17(7):538-51

2017, 7(1):1899

Catalog No. Information Product Use Citations Product Validations
S3042

Purmorphamine

Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

2017, 50(2):373-380

2017, 36(1):23

2017, 7(1):1899

S7779

Smoothened Agonist (SAG) HCl

Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

2013, 58(5):1801-13

Tags: Smo activity | smoothened pathway | smoothened pathway | smoothened signaling | Smo cancer | Smo pathway | smoothened signaling pathway | smoothened inhibitor review